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Saracatinib

CAS No. : 379231-04-6

MCE 站：Saracatinib

产品活性：Saracatinib (AZD0530) 是一种有效的 Src 抑制剂，抑制 c-Src，Lck，c-YES，Lyn，Fyn，Fgr 和 Blk 的 IC₅₀ 值为 2.7-11 nM，对其他酪氨酸激酶具有选择性。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：Src  |  Autophagy

In Vitro: Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC₅₀ of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC₅₀ values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC₅₀ of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC₅₀ 0.14 μM).

In Vivo: Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats).

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Bosutinib  |  PP2  |  SU6656  |  Src Inhibitor 1  |  WH-4-023  |  Pelitinib  |  Scutellarein  |  PP1  |  1-Naphthyl PP1  |  1-NM-PP1  |  Lck Inhibitor  |  RK-24466  |  Tolimidone  |  A-770041  |  PP121  |  PP58  |  PD173955  |  MNS  |  AZM475271  |  7-Hydroxy-4H-chromen-4-one  |  β-Hydroxyisovalerylshikonin  |  PD-161570  |  UM-164  |  CGP77675  |  Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH  |  Caffeic acid-pYEEIE TFA

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